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A series of novel derivatives of 4, 5, 6, 7-tetrahydrothieno [3,2-c] pyridine were synthesized and structurally characterized by 1H NMR and MS. Their in vivo anti-platelet aggregation activities were evaluated. A 3D-QSAR was performed using the CoMFA and the CoMSIA. This model provided useful guidelines for novel anti-platelet thienopyridines design. 相似文献
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YuHanZHOU WeiRongMIAO LuBaiCHEN 《中国化学快报》2003,14(9):897-900
Several novel 3-(substituted phenyl)isoxazole derivatives were prepared from phenyl butan-l,3-dione. Their structures were confirmed by IH NMR, 1R, and CIMS. Preliminary bioassay showed that some of them exhibited good activities toward various weeds. 相似文献
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Xin Ying ZHANG Yan Zhen LI Xue Sen FAN Gui Rong QU Xue Yuan HU Jian Ji WANG 《中国化学快报》2006,17(2):150-152
1, 4-Dihydropyridine (DHP) heterocyclic ring is a common feature of various bioactivecompounds such as vasodilator, bronchodilator and antiatherosclerotic, antitumor, andantidiabetic agents1. Due to their important pharmacological activities, many methods… 相似文献
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ZHENG Zhan-Ying SONG Hai-Bin TONG Jun YAN Dong-Wen LI Zheng-Ming CHEN Jian-Yu ZHANG Shu-Jun LIU Xing-Hai WANG Su-Hua 《结构化学》2008,27(7):841-845
ABSTRACT Monosulfuron is a novel sulfonylurea herbicide with ultra-low dosage invented and patented by Nankai University. Herein its sodium salt was firstly synthesized and crystal structure was determined by X-ray diffraction method. The title compound belongs to the triclinic system, space group P1^- with a = 7.306(6), b = 9.446(8), c = 11.872(10)A, α = 76.578(14), β = 78.049(13), γ = 77.620(14)°, V = 767.7(11)A^3, Mr = 377.32, Z = 2, Dc = 1.632 g/cm^3,μ= 0.283 mm^-1, F(000) = 388, R = 0.0444 and wR = 0.1186. In the title compound, Na(1) coordinates with 0(4) and 0(5) from one monosulfuron molecule, N(4A) and O(5A) from the other monosulfuron molecule and the oxygen atom from H2O to give five coordination bonds. The title complex is further linked into a three-dimensional structure through π…π interactions and intermolecular hydrogen bonds between the oxygen and nitrogen atoms. 相似文献
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1INTRODUCTION Pyrazolo[1,5-a]pyrimidine derivatives have shown various biological activities in the terms of antibac-terial,antischistosomal and xanthine oxidase inhibi-tors[1~5].The enaminones are highly reactive inter-mediates and have been extensively used as build-ing blocks in organic synthesis especially in the he-terocyclic compounds[6~8].In addition,a great deal of interest has been focused on the synthesis of py-razolo[1,5-a]pyrimidine through versatile enamino-nes because of thei… 相似文献
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Khalil Faghihi 《中国化学快报》2009,20(10):1153-1156
Six new optically active poly(amide-imide)s(5a-f) were synthesized through the direct polycondensation reaction of N,N'-(4,4'- diphthaloyl)-bis-L-leucine(3) with six hydantoin derivatives(4a-f).Triphenyl phosphite(TPP)/pyridine in the presence of calcium chloride(CaCl_2) and N-methyl-2-pyrrolidone(NMP) were successfully applied for direct polycondensation.The polycondensation reactions produce a series of new poly(amide-imide)s(5a-f) in high yields,and inherent viscosity between 0.42 and 0.55 dL/g.The re... 相似文献
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Zhi Yong Tian Hong Xia Ma Song Qiang Xie Xue Wang Jin Zhao Chao Jie Wang Wen Yuan Gao 《中国化学快报》2008,19(5):509-512
Two novel mononaphthalimide homospermidine derivatives (2a, 2b) with three or four methylene unit as linkages were synthesized and evaluated for cytotoxicity against human leukemia K562, murine melanoma B 16 and Chinese hamster ovary CHO cell lines. The presence of homospermidine motif could greatly elevate the potency of 1,8-naphthalimide. Conjugate 2b with longer spacer exhibited higher in vitro cytotoxicity than 2a. The DNA binding experiments indicated that conjugates 2b could bind to herring sperm DNA. The topoisomerase Ⅱ poison trials revealed that 2b could inhibit the activity of top. Ⅱ. 相似文献
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A novel compound 4,8,10-trimethyl-2-(3,5-dimethylpyrazol)-pyrido-[2',3':3,4]-py-razol-[1,5-5-a]-pyrimidine(C17H18N6) has been synthesized from 2,6-dichloro-4-methylnico-tino-nitrile,hydrazine and acetylacetone by substitution and cyclolization.The structure was charac-terized by elemental analysis,1H NMR and IR,and single-crystal structure was determined by X-ray diffraction analysis.The compound crystallizes in the monoclinic system,space group P21/c with a = 8.0338(9),b = 28.618(3),c = 7.2688(8),β = 111.051(2)o,V = 1559.6(3) 3,Z = 4,Dc = 1.305 g/cm3,μ = 0.083 mm-1,Mr = 306.37,F(000) = 648,S = 0.971,the final R = 0.0795 and wR = 0.1746 for 1457 observed reflections(Ⅰ 2σ(Ⅰ)).The results demonstrate that the pyridine,pyrazole and pyrimidine rings are nearly coplanar,which is evident from the dihedral angles among the four rings in the range of 0.13~4.15o.The face-to-face π-π stacking interactions among pyridine,pyrazol and pyrimidine rings result in a supramolecular crystal,in which they seem to be effective in stabilizing the structure.Meanwhile,the fluorescence properties of the title compound were discussed,which showed very strong fluorescence.The calculated results(selected bond lengths,bond angles and torsion angles) are all typical and agree well with the experimental results,which demonstrates that B3LYP/6-31+G* is suitable for the title compound. 相似文献
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ZHANG Ting-Ting JU Yan-Ling WANG Chun-Yan LI Yan-Qiu LI Xia 《结构化学》2007,26(7):838-842
The complex [Eu(3-IBA)3·2,2'-bipy]2 was synthesized from 3-iodobenzoic acid (3-HIBA), 2,2'-bipyridine (2,2‘-bipy) and EuCl3·6H2O by hydrothermal synthesis, and its crystal structure was determined by X-ray single-crystal diffraction. It is of triclinic, space group Pi, with a = 10.958(2), b = 12.311(3), c = 12.556(3) A, α = 81.549(3), β = 82.404(4), γ = 78.348(3)°, Mr = 1049.15, V= 1631.7(6) A3, Z = 1, Dc = 2.135 g/cm^3, F(000) = 980, 2(MoKa) = 0.71073 A,μ(MoKa) = 4.804 mm^-1, the final R = 0.0329 and wR = 0.0723 for 4640 observed reflections with I 〉 2σ(I). The Eu(Ⅲ) ion is eight-coordinated and two Eu(Ⅲ) ions are held together by four 3-iodobenzoate groups in the bidentate bridging mode. The complex was characterized by DTA-TG, IR, UV and fluorescence spectra. 相似文献
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HUANG Qiang FU Qiangqiang LIU Yajing BAI Jinying WANG Qianying LIAO Huimin GONG Ping 《高等学校化学研究》2014,30(2):257-265
In an attempt to develop potent and selective anticancer agents,we designed and synthesized a series of novel bis(morpholino-1,3,5-triazine) derivatives beating aylmethylene hydrazine moiety and evaluated their cytotoxicity,in vitro,against H460(non-small-cell lung cancer),HT-29(human colorectal cancer) and MDA-MB-231(human breast cancer) cell lines.The pharmacological results indicate that all the compounds exhibit enhanced cytotoxicity than BMCL-200908069-1,and six target compounds(7e,7h,7j,9a,9b,9c) were superior to PAC-1 against all the tested cancer cell lines.The most active compound 7j,with IC50(inhibitory concentration 50%)values of 0.75,0.34 and 0.60 μ mol/L against HT-29,H460 and MDA-MB-231 cancer cell lines,was 39-,28-,and 60-fold more potent than BMCL-200908069-1 (29.24,9.52 and 36.21 μmol/L),respectively. 相似文献
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A new series of quinazolin-4(3H)-one derivatives containing a(1 3-diphenyl-1H-pyrazol-4-yl) core with substituents at the 2-position and aromatic or heteroaromatic substituents at the 3-position were synthesized using an L-proline catalyzed one-pot multi-component reaction approach.All the synthesized compounds were characterized and screened for their antimicrobial,antifungal and anti-tubercular activities. 相似文献
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Xian Ping DAI Xing Zhou LI Zhi Bing ZHENG Song LI 《中国化学快报》2006,17(5):609-612
Many diaryl or triaryl substituted imidazoles and triazoles are known to be selective inhibitors of transforming growth factor β1(TGF-β1) type 1 receptor (ALK5)1-3. SB-431542, one of the leading compound of 2-pyridyl substituted triarylimidazole, is an … 相似文献
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A series of pyrazole[3,4-d] pyrimidin-4-one derivatives were synthesized and tested for vasodilatory activities. All of them were new compounds and their structures were confirmed by IR,^1H NMR,MS and elemental analysis. 相似文献
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Dong-Mei Zhao Wen-Yan Li Yu-Fang Shi Xu-Qiong Xiong Shuai Song Chen-Zhou Ha Mao-Sheng Cheng Jing-Kang Shen 《中国化学快报》2014,25(2):299-304
Cholesteryl ester transfer protein (CETP) is a plasma glycoprotein that plays an important role in decreasing high-density lipoprotein cholesterol (HDL-C) levels and increasing low-density lipoprotein cholesterol (LDL-C) levels. Inhibition of CETP may be a new therapy for treating atherosclerosis. Herein, we report the development of a ligand-based pharmacophore model and pharmacophore-based virtual screening of the ZINC/big-n-greasy database, leading to the identification of compound H-10 as a potential CETP inhibitor in vitro. Based on H-10, a series of 3-((3,4-dichlorophenyl)(4-substituted benzyl)amino) propanamides were designed, synthesized, and evaluated against CETP. Compound 41 was found to have the best activity, resulting in 85.0% inhibition of CETP at l0 μmol/L. 相似文献
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The title Schiff base compound (C11H8N4O), a derivative of pyrazole, has been synthesized by the reaction of salicylaldehyde and 3-amino-4-cyanopyrazole in absolute ethanol and characterized by elemental analyses, IR, ^1H NMR and X-ray single-crystal diffraction. The crystal belongs to the monoclinic system, space group P21/n, with a = 7.5594(7), b = 18.3342(19), c = 22.461(2) A^°, β = 98.419(2)°, V = 3079.5(5) A^°3, Mr = 212.21, Z = 12, F(000) = 1320, Dc = 1.373 g/cm^3, T = 298(2) K, 2 = 0.71073 A^°, the final R = 0.0571 and wR = 0.0493. A total of 5412 unique reflections were collected, of which 1612 with I 〉 2σ(I) were observed. The molecular structure adopts a trans configuration about the C=N double bond. The preliminary biological tests show that the compound has high antibacterial activities. 相似文献